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Last Updated: December 22, 2024

Claims for Patent: 5,344,932

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Summary for Patent: 5,344,932

Title:	N-(pyrrolo(2,3-d)pyrimidin-3-ylacyl)-glutamic acid derivatives
Abstract:	N-(Acyl)glutamic acid derivatives in which the acyl group is substituted with 4-hydroxypyrrolo[2,3-d]-pyrimidin-3-yl group are antineoplastic agents. A typical embodiment is N-[4-(2-{4-hydroxy-6-aminopyrrolo-[2,3-d]pyrimidin-3-yl}ethyl)benzoyl]-L-g lutamic acid.
Inventor(s):	Taylor; Edward C. (Princeton, NJ)
Assignee:	Trustees of Princeton University (Princeton, NJ)
Application Number:	07/674,541
Patent Claims:	1. A compound of the formula: ##STR14## in which: R.sup.1 is --OH or --NH.sub.2 ; R.sup.2 is hydrogen or a pharmaceutically acceptable cation: R.sup.3 is 1,4-phenylene unsubstituted or substituted with chloro, fluoro, methyl, methoxy, or trifluoromethyl; R.sup.4 is hydrogen, or methyl; R.sup.5 is amino; and the configuration about the carbon atom designated * is S. 2. A compound according to claim 1 wherein R.sup.1 is --OH; R.sup.3 is 1,4-phenylene, and R.sup.4 is hydrogen. 3. The compound according to claim 1 which is N-{4-[2-(4-hydroxy-6-aminopyrrolo[2,3-d]pyrimidin-3-yl)ethyl]benzoyl}-L-gl utamic acid. 4. The compound according to claim 1 which is N-{4-[1-hydroxy-3-(4-hydroxy-6-aminopyrrolo[2,3-d]pyrimidin-3-yl)prop-2-yl ]benzoyl}glutamic acid. 5. The compound according to claim 1 which is N-{2-fluoro-4-[2-(4-hydroxy-6-aminopyrrolo[2,3-d]pyrimidin-3-yl)ethyl]benz oyl}-L-glutamic acid. 6. The compound according to claim 1 which is N-{3-fluoro-4-[2-(4-hydroxy-6-aminopyrrolo[2,3-d]pyrimidin-3-yl)ethyl]benz oyl}-L-glutamic acid. 7. A compound of the formula: ##STR15## in which: R.sup.1 is --OH or --NH.sub.2 ; R.sup.2' is hydrogen, a pharmaceutically acceptable cation, or a carboxy protecting group: R.sup.3 is 1,4-phenylene unsubstituted or substituted with chloro, fluoro, methyl, methoxy, or trifluoromethyl; R.sup.4' is hydrogen, or methyl; R.sup.5' is amino or amino substituted with an amino protecting group; and the configuration about the carbon atom designated * is S.

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